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TWI310766B - Solid salt forms of a pyrrole substituted 2-indolinone - Google Patents

Solid salt forms of a pyrrole substituted 2-indolinone Download PDF

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Publication number
TWI310766B
TWI310766B TW095134445A TW95134445A TWI310766B TW I310766 B TWI310766 B TW I310766B TW 095134445 A TW095134445 A TW 095134445A TW 95134445 A TW95134445 A TW 95134445A TW I310766 B TWI310766 B TW I310766B
Authority
TW
Taiwan
Prior art keywords
compound
phosphate
solvent
solution
allotrope
Prior art date
Application number
TW095134445A
Other languages
English (en)
Chinese (zh)
Other versions
TW200745093A (en
Inventor
Changquan Calvin Sun
Michael Hawley
Original Assignee
Pfizer Prod Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of TW200745093A publication Critical patent/TW200745093A/zh
Application granted granted Critical
Publication of TWI310766B publication Critical patent/TWI310766B/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW095134445A 2005-09-19 2006-09-18 Solid salt forms of a pyrrole substituted 2-indolinone TWI310766B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US71858605P 2005-09-19 2005-09-19

Publications (2)

Publication Number Publication Date
TW200745093A TW200745093A (en) 2007-12-16
TWI310766B true TWI310766B (en) 2009-06-11

Family

ID=37626412

Family Applications (1)

Application Number Title Priority Date Filing Date
TW095134445A TWI310766B (en) 2005-09-19 2006-09-18 Solid salt forms of a pyrrole substituted 2-indolinone

Country Status (24)

Country Link
US (3) US20080275101A1 (ru)
EP (2) EP1928858B1 (ru)
JP (2) JP4519114B2 (ru)
KR (1) KR101050906B1 (ru)
CN (2) CN103601720B (ru)
AR (1) AR056521A1 (ru)
AU (1) AU2006293644B2 (ru)
BR (1) BRPI0616374B8 (ru)
CA (1) CA2621569C (ru)
CY (1) CY1109326T1 (ru)
DE (1) DE602006008015D1 (ru)
DK (1) DK1928858T3 (ru)
ES (1) ES2328407T3 (ru)
IL (1) IL189590A0 (ru)
MX (1) MX2008002415A (ru)
NO (1) NO20080866L (ru)
NZ (1) NZ566033A (ru)
PL (1) PL1928858T3 (ru)
PT (1) PT1928858E (ru)
RU (1) RU2399619C2 (ru)
SI (1) SI1928858T1 (ru)
TW (1) TWI310766B (ru)
WO (1) WO2007034272A1 (ru)
ZA (1) ZA200801431B (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1928858T3 (da) 2005-09-19 2009-10-26 Pfizer Prod Inc Faste saltformer af et pyrrolsubstitueret 2-indolinon
US20100189788A1 (en) 2009-01-23 2010-07-29 Teva Pharmaceutical Industries, Ltd. Delayed release rasagiline base formulation
CN102858739A (zh) 2010-03-10 2013-01-02 斯索恩有限公司 酰胺化吡咯甲酸酯化合物的方法

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2155187C2 (ru) * 1992-08-06 2000-08-27 Варнер-Ламберт Компани Производные индола, их таутомеры, смеси их изомеров или отдельные изомеры и фармацевтически приемлемые соли, фармацевтическая композиция с антиопухолевой или ингибирующей протеин-тирозинкиназу активностью и способ торможения зависящего от протеин-тирозинкиназы заболевания или борьбы с аберрантным ростом клеток млекопитающего или человека.
US6574293B1 (en) 1998-10-28 2003-06-03 Ericsson Inc. Receivers and methods for reducing interference in radio communications
PT1255536E (pt) * 1999-12-22 2006-09-29 Sugen Inc Derivados de indolinona para a modulacao da tirosina proteina cinase de tipo c-kit
PT1255752E (pt) * 2000-02-15 2007-10-17 Pharmacia & Upjohn Co Llc Inibidores de proteína quinases: 2-indolinonas substituídas com pirrolo
WO2002081466A1 (en) * 2001-04-09 2002-10-17 Sugen, Inc. Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
DK3168218T3 (en) 2001-08-15 2019-01-14 Pharmacia & Upjohn Co Llc Crystalline comprising an L-malic acid salt of N- [2- (DIETHYLAMINO) ETHYL] -5 - [(5-FLUOR-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDE) METHYL] -2,4 -DIMETHYL-1H-PYRROL-3-CARBOXAMIDE FOR USE AS A MEDICINE
MXPA04006992A (es) * 2002-02-15 2004-11-10 Upjohn Co Procedimiento para preparar derivados de indolinona.
US7452913B2 (en) * 2003-02-24 2008-11-18 Pharmacia & Upjohn Company Polymorphs of pyrrole substituted 2-indolinone protein kinase inhibitors
US20040209937A1 (en) * 2003-02-24 2004-10-21 Sugen, Inc. Treatment of excessive osteolysis with indolinone compounds
US20060009510A1 (en) * 2004-07-09 2006-01-12 Pharmacia & Upjohn Company Llc Method of synthesizing indolinone compounds
DK1928858T3 (da) 2005-09-19 2009-10-26 Pfizer Prod Inc Faste saltformer af et pyrrolsubstitueret 2-indolinon

Also Published As

Publication number Publication date
DE602006008015D1 (de) 2009-09-03
JP2007084540A (ja) 2007-04-05
CN103601720A (zh) 2014-02-26
AU2006293644A1 (en) 2007-03-29
RU2008109959A (ru) 2009-10-27
BRPI0616374B8 (pt) 2021-05-25
NO20080866L (no) 2008-03-13
TW200745093A (en) 2007-12-16
IL189590A0 (en) 2008-08-07
EP1928858A1 (en) 2008-06-11
BRPI0616374B1 (pt) 2020-05-12
CN101287724A (zh) 2008-10-15
US20080275101A1 (en) 2008-11-06
PT1928858E (pt) 2009-09-17
PL1928858T3 (pl) 2009-12-31
ZA200801431B (en) 2009-07-29
EP2112148A1 (en) 2009-10-28
KR20080037093A (ko) 2008-04-29
AR056521A1 (es) 2007-10-10
ES2328407T3 (es) 2009-11-12
US9290479B2 (en) 2016-03-22
CN103601720B (zh) 2016-08-10
EP1928858B1 (en) 2009-07-22
AU2006293644B2 (en) 2012-05-31
SI1928858T1 (sl) 2009-10-31
BRPI0616374A2 (pt) 2011-06-21
CA2621569A1 (en) 2007-03-29
US20150158849A1 (en) 2015-06-11
HK1125101A1 (en) 2009-07-31
NZ566033A (en) 2011-04-29
CN101287724B (zh) 2013-11-06
DK1928858T3 (da) 2009-10-26
CA2621569C (en) 2010-10-19
CY1109326T1 (el) 2014-07-02
JP4519114B2 (ja) 2010-08-04
MX2008002415A (es) 2008-03-27
WO2007034272A1 (en) 2007-03-29
JP2010090152A (ja) 2010-04-22
US8987320B2 (en) 2015-03-24
US20120142749A1 (en) 2012-06-07
KR101050906B1 (ko) 2011-07-20
RU2399619C2 (ru) 2010-09-20

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